The present invention relates to a percutaneous absorption accelerator and a percutaneous absorbent preparation containing the same, and more particularly, to a percutaneous absorption accelerator containing ether derivatives of specific glycerols or polyglycerols and alcohols as the active ingredients and percutaneous absorbent accelerators and pharmaceutically effective components.
As methods for administration of drugs, oral administration, rectal administration, intracutaneous administration, and so forth have been generally adopted. Among these, oral administration has been widely employed. However, in the case of oral administration, certain difficulties have been encountered due to side effects such as gastrointestinal disturbances, anorexia, vomitting, and abdominal pain. In addition it is necessary in most cases to administer large quantities of these drugs. In recent years, preparations for percutaneous administration have been developed, some have been for, commercial use, in hopes that the side effects would be minimized and the desired pharmacological effects would occur more safely. In many cases, however, percutaneo absorbability of pharmaceutically effective components in such preparations are unsatisfactory and the purposes have been satisfactorily achieved only with difficulty. Namely, skin and its keratin layer (which constitutes the outermost layer) functions physiologically and acts as a protective wall against permeation of substances into the body. In many cases, it is difficult for a base alone, used for conventional topical agents, to attain percutaneous absorption sufficient for the pharmaceutically components formulated therein to be effective. For this reason, a device is necessary to control the permeability of drugs through the keratin layer of the skin and enhance the percutaneous absorption of drugs.
In addition, for accelerating absorption of pharmacologically active substances from the mucous portions of the human body, such as the mucous membrane of the eye, nasal mucous membrane, bucal mucous membrane, vaginal mucous membrane, rectal mucous membrane, improvement of the preparation form, improvement of bases, formulation of compounds having an absorption acceleration effect, and the like have been made. Among them, the improvement of the preparation form and the improvement of bases are possible to a certain extent; however, epochmaking improvement is not expected and the target of research has been focused on the search for and application of compounds having an absorption accelerating effect.
For such purposes, it has generally been known to formulate a so called percutaneous absorption accelerator in a base. As such absorption accelerators, there are known dimethyl sulfoxide; amide compounds such as dimethyl acetamide, dimethylformamide, and N,N-diethyl-m-toluamide, azacycloalkan-2-one derivatives, such as 1-dodecylazacyclo-heptan-2-one; esters of alcohol and carboxylic acids, such as isopropyl myristate, isopropyl palmitate, diethyl sebacate, and diisopropyl adipate; and crotonyl-N-ethyl-o-toluidine. However, these absorption accelerators have been found to be unsatisfactory in their absorption accelerating effect and, in many cases, practical pharmacological effects cannot be obtained. In addition, these pharmacological effects cannot be obtained. Moreover, these absorption accelerators involve problems in practical use because the absorption accelerators themselves show irritation to the skin and corrode synthetic resins due to their property as potent solvents to dissolve irritative substances, and sensitized substances out of containers for drugs, clothes, and accessories, so that general adaptation and use are restricted.